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Nilotinib oral preparation

An oral preparation, nilotinib technology, applied in the field of pharmaceutical preparations, can solve the problems of difficult release of drugs, inability to improve dissolution and bioavailability, etc., and achieve the effects of improving bioavailability, improving stability, and improving safety.

Active Publication Date: 2015-01-14
FERGUSON WUHAN BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] However, we found in our research that after inclusion of nilotinib with cyclodextrin, although the solubility of nilotinib can be improved, its dissolution rate and bioavailability cannot be improved. The reason may be that nilotinib The binding force between tinib and cyclodextrin molecules is strong, and cyclodextrin and nilotinib form a tight combination, which makes it difficult for the drug to be released from the molecular cavity of cyclodextrin

Method used

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  • Nilotinib oral preparation
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  • Nilotinib oral preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Nilotinib tablets, made from the following raw materials:

[0029]

[0030] The preparation method is:

[0031] 1) Preparation of nilotinib inclusion compound (saturated aqueous solution method)

[0032] Weigh 0.6g of tryptophan and 400g of hydroxypropyl-β-cyclodextrin, place them in a 1000ml three-necked bottle with an electric stirring device, add 500ml of water, and put them in a water bath at 40°C to dissolve them; weigh nilotinib 50g, dissolve with 70ml ethanol, drop it into the saturated solution of hydroxypropyl-β-cyclodextrin, stir at constant temperature for 6 hours, let it stand for precipitation, filter with suction, wash the precipitate with an appropriate amount of ethanol, and vacuum at 50°C Dry to obtain nilotinib inclusion compound.

[0033] 2) Preparation of tablets

[0034] Add 6 g of hydroxypropyl cellulose to 50% ethanol to make a solution with a concentration of 2%, mix the nilotinib inclusion complex with 72 g of lactose, and then use the hyd...

Embodiment 2

[0037] Nilotinib tablets, made from the following raw materials:

[0038]

[0039]

[0040] The preparation method is:

[0041] 1) Preparation of nilotinib inclusion compound (solution-stirring method)

[0042] Weigh 0.35g of tryptophan and 250g of hydroxypropyl-β-cyclodextrin, put them in a beaker, add 1000ml of water, stir and dissolve; take 50g of nilotinib, dissolve with ethanol and slowly add to the above-mentioned hydroxypropyl-β-cyclodextrin In the mixed aqueous solution of β-cyclodextrin and tryptophan, the mixed solution was stirred by magnetic stirring for 20 minutes until the solution was completely clear; the clarified solution was rotary evaporated, and after drying, the nilotinib inclusion compound was obtained.

[0043] 2) Preparation of tablets

[0044] Add 3 g of hydroxypropyl cellulose to 50% ethanol to make a solution with a concentration of 2%, mix the nilotinib inclusion complex with 60 g of lactose, and then use the hydroxypropyl cellulose solutio...

Embodiment 3

[0046] Nilotinib capsules, made from the following raw materials:

[0047]

[0048] The preparation method is:

[0049] 1) Preparation of nilotinib inclusion compound

[0050] Prepared by solution-stirring method.

[0051] 2) Preparation of capsules

[0052] Mix the nilotinib inclusion compound prepared in step 1) with silicon dioxide and magnesium stearate, and fill it with capsules.

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Abstract

The invention discloses a nilotinib oral preparation. The preparation contains an effective dose of nilotinib, hydroxypropyl-beta-cyclodextrin and tryptophan in a mass ratio of 1:(5-24):(0.007-0.02), wherein nilotinib and tryptophan are included in the molecular cavity of hydroxypropyl-beta-cyclodextrin. According to the nilotinib oral preparation, the solubility and dissolution rate of nilotinib in the preparation can be effectively improved, the bioavailability of nilotinib can be improved, the stability of nilotinib can be improved, and the safety of the preparation can be improved.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to an oral nilotinib preparation. Background technique [0002] The tyrosine kinase inhibitor imatinib (imatinib) is currently the first-line standard treatment for chronic myeloid leukemia (CML). It can target the BCR-ABL fusion protein and greatly improve the course and prognosis of CML. However, The occurrence of drug resistance and the inability to completely eradicate the disease limit its curative effect. Nilotinib, a second-generation tyrosine kinase inhibitor, has higher affinity and specificity for BCR-ABL than imatinib. Nilotinib has been approved for the treatment of imatinib-resistant or intolerant CML patients in chronic phase (CP) and accelerated phase (AP) in most countries around the world, including China, and was officially approved by the US FDA in June 2010 Nilotinib is used in the first-line treatment of CML. Clinical studies of nilotinib in patient...

Claims

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Application Information

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IPC IPC(8): A61K47/48A61K47/22A61K31/506A61P35/02
Inventor 欧阳康乐赵小伟黄飞牛彬彬饶又启
Owner FERGUSON WUHAN BIOTECH